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We study how to generate molecule conformations (i.e., 3D structures) from a molecular graph. Traditional methods, such as molecular dynamics, sample conformations via computationally expensive simulations. Recently, machine learning…

Machine Learning · Computer Science 2021-04-01 Minkai Xu , Shitong Luo , Yoshua Bengio , Jian Peng , Jian Tang

The de novo design of molecular structures using deep learning generative models introduces an encouraging solution to drug discovery in the face of the continuously increased cost of new drug development. From the generation of original…

Biomolecules · Quantitative Biology 2021-02-08 Yuemin Bian , Xiang-Qun Xie

Designing new chemical compounds with desired pharmaceutical properties is a challenging task and takes years of development and testing. Still, a majority of new drugs fail to prove efficient. Recent success of deep generative modeling…

Machine Learning · Computer Science 2021-09-15 Karina Zadorozhny , Lada Nuzhna

It is common practice for chemists to search chemical databases based on substructures of compounds for finding molecules with desired properties. The purpose of de novo molecular generation is to generate instead of search. Existing…

Chemical Physics · Physics 2021-02-10 Ryuichiro Hataya , Hideki Nakayama , Kazuki Yoshizoe

Molecular generation and molecular property prediction are both crucial for drug discovery, but they are often developed independently. Inspired by recent studies, which demonstrate that diffusion model, a prominent generative approach, can…

Machine Learning · Computer Science 2025-04-07 Shikun Feng , Yuyan Ni , Yan Lu , Zhi-Ming Ma , Wei-Ying Ma , Yanyan Lan

Recent advances in machine learning for molecules exhibit great potential for facilitating drug discovery from in silico predictions. Most models for molecule generation rely on the decomposition of molecules into frequently occurring…

Chemical Physics · Physics 2023-11-08 Leon Hetzel , Johanna Sommer , Bastian Rieck , Fabian Theis , Stephan Günnemann

Searching new molecules in areas like drug discovery often starts from the core structures of candidate molecules to optimize the properties of interest. The way as such has called for a strategy of designing molecules retaining a…

Machine Learning · Computer Science 2020-09-03 Jaechang Lim , Sang-Yeon Hwang , Seungsu Kim , Seokhyun Moon , Woo Youn Kim

Molecular dynamics (MD) is a powerful technique for studying microscopic phenomena, but its computational cost has driven significant interest in the development of deep learning-based surrogate models. We introduce generative modeling of…

Biomolecules · Quantitative Biology 2024-09-27 Bowen Jing , Hannes Stärk , Tommi Jaakkola , Bonnie Berger

Generating new molecules with specified chemical and biological properties via generative models has emerged as a promising direction for drug discovery. However, existing methods require extensive training/fine-tuning with a large dataset,…

Quantitative Methods · Quantitative Biology 2023-04-25 Zichao Wang , Weili Nie , Zhuoran Qiao , Chaowei Xiao , Richard Baraniuk , Anima Anandkumar

Molecule generation is central to a variety of applications. Current attention has been paid to approaching the generation task as subgraph prediction and assembling. Nevertheless, these methods usually rely on hand-crafted or external…

Machine Learning · Computer Science 2022-12-20 Xiangzhe Kong , Wenbing Huang , Zhixing Tan , Yang Liu

Molecule optimization is a fundamental task for accelerating drug discovery, with the goal of generating new valid molecules that maximize multiple drug properties while maintaining similarity to the input molecule. Existing generative…

Machine Learning · Computer Science 2024-07-02 Tianfan Fu , Cao Xiao , Xinhao Li , Lucas M. Glass , Jimeng Sun

The integration of artificial intelligence (AI) in early-stage drug discovery offers unprecedented opportunities for exploring chemical space and accelerating hit-to-lead optimization. However, docking optimization in generative approaches…

Quantitative Methods · Quantitative Biology 2025-10-03 Ekaterina Podplutova , Anastasia Vepreva , Olga A. Konovalova , Vladimir Vinogradov , Dmitrii O. Shkil , Andrei Dmitrenko

The goal of structure-based drug discovery is to find small molecules that bind to a given target protein. Deep learning has been used to generate drug-like molecules with certain cheminformatic properties, but has not yet been applied to…

Quantitative Methods · Quantitative Biology 2022-01-27 Matthew Ragoza , Tomohide Masuda , David Ryan Koes

Deep generative models of molecules have grown immensely in popularity, trained on relevant datasets, these models are used to search through chemical space. The downstream utility of generative models for the inverse design of novel…

Machine Learning · Computer Science 2023-05-11 Daniel Flam-Shepherd , Kevin Zhu , Alán Aspuru-Guzik

Molecule generation is a challenging open problem in cheminformatics. Currently, deep generative approaches addressing the challenge belong to two broad categories, differing in how molecules are represented. One approach encodes molecular…

Machine Learning · Statistics 2020-11-02 Marco Podda , Davide Bacciu , Alessio Micheli

Despite recent advances, goal-directed generation of structured discrete data remains challenging. For problems such as program synthesis (generating source code) and materials design (generating molecules), finding examples which satisfy…

Machine Learning · Computer Science 2020-10-26 Amina Mollaysa , Brooks Paige , Alexandros Kalousis

Discovering functional crystalline materials entails navigating an immense combinatorial design space. While recent advances in generative artificial intelligence have enabled the sampling of chemically plausible compositions and…

Machine Learning · Computer Science 2025-11-11 Hyunsoo Park , Aron Walsh

Molecular generation, an essential method for identifying new drug structures, has been supported by advancements in machine learning and computational technology. However, challenges remain in multi-objective generation, model…

Biomolecules · Quantitative Biology 2024-04-11 Ningfeng Liu , Jie Yu , Siyu Xiu , Xinfang Zhao , Siyu Lin , Bo Qiang , Ruqiu Zheng , Hongwei Jin , Liangren Zhang , Zhenming Liu

By linking conceptual theories with observed data, generative models can support reasoning in complex situations. They have come to play a central role both within and beyond statistics, providing the basis for power analysis in molecular…

Methodology · Statistics 2022-08-15 Kris Sankaran , Susan P. Holmes

Recent advancements in large language models (LLMs) have demonstrated impressive performance in molecular generation, which offers potential to accelerate drug discovery. However, the current LLMs overlook a critical requirement for drug…

Machine Learning · Computer Science 2025-02-18 Hyosoon Jang , Yunhui Jang , Jaehyung Kim , Sungsoo Ahn